Wirkstoffe M Mechlorethamine Megestrol MEK 162 Melphalan
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Glossary A-Z V Z T U R W P Q Wirkstoffe M N O L M I K G H Magrolimab/ anti-CD47 monoclonal E antibody F Hu5F9-G4 C D Navigation überspringen A B According to the NCI website, Magrolimab is a humanized monoclonal antibody targeting the human cell surface antigen CD47, with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD47 monoclonal antibody Hu5F9-G4 selectively binds to CD47 expressed on tumor cells and blocks the interaction of CD47 with its ligand signal regulatory protein alpha (SIRPa), a protein expressed on phagocytic cells. This prevents CD47/SIRPa-mediated signaling, allows the activation of macrophages, through the induction of pro-phagocytic signaling mediated by calreticulin, which is specifically expressed on the surface of tumor cells, and results in specific tumor cell phagocytosis. In addition, blocking CD47 signaling activates an anti-tumor T-lymphocyte immune response and T-cell mediated cell killing. CD47, a tumor associated antigen expressed on normal, healthy hematopoietic stem cells (HSC), is overexpressed on the surface of a variety of cancer cells. Expression of CD47, and its interaction with SIRP-alpha, leads to inhibition of macrophages and protects cancer cells from phagocytosis thereby allowing cancer cells to proliferate. Check for active clinical trials using this agent. (NCI Thesaurus) More Information in English: Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health Link to National Cancer Institute Margetuximab According to the NCI website, margetuximab is a Fc-domain optimized IgG monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2) with potential immunomodulating and antineoplastic activities. After binding to HER2 on the tumor cell surface, margetuximab may induce an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells overexpressing HER2. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types. Compared to other anti-HER2 monoclonal antibodies, the Fc domain of MGAH22 is optimized with increased binding to the activating Fcgamma receptor IIIA (CD16A), expressed on cells such as natural killer (NK) cells and macrophages, thereby mediating an enhanced ADCC; the Fc domain also shows decreased binding to the inhibitory Fcgamma receptor IIB (CD32B). Check for active clinical trials using this agent. (NCI Thesaurus) More Information in English: Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health Link to National Cancer Institute Wiki MBG453 - Anti-TIM-3 Monoclonal Antibody According to the NCI website, MBG453 (Anti-TIM-3 Monoclonal Antibody MBG453) is an inhibitor of the inhibitory T-cell receptor T-cell immunoglobulin and mucin domain-containing protein 3 (TIM-3; hepatitis A virus cellular receptor 2; HAVCR2), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, the anti-TIM-3 checkpoint inhibitor MBG453 binds to TIM-3 expressed on certain immune cells, including tumor infiltrating lymphocytes (TILs). This abrogates T-cell inhibition, activates antigen-specific T-lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis resulting in a reduction in tumor growth. TIM-3, a transmembrane protein expressed on certain T-cells, is associated with tumor-mediated immune suppression. Link to National Cancer Institute Wiki Relationships with other NCI Thesaurus Concepts MGD013 - anti-PD-1/anti-LAG-3 DART protein According to the NCI website, MGD013 is an Fc-bearing, humanized antibody-like protein that specifically recognizes the immune checkpoint molecules programmed cell death 1 (PD-1; PD1; PDCD1; CD279; Programmed Death 1) and lymphocyte activation gene-3 (LAG-3; LAG3; CD223), with potential T-lymphocyte immunomodulatory and antineoplastic activities. Upon administration, the anti-PD-1/anti- LAG-3 dual-affinity re-targeting (DART) protein MGD013 specifically binds to both PD-1 and LAG-3, which are both expressed on T cells. The dual blockade of the PD-1 and LAG-3 pathways enables potent activation of a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. PD-1 and LAG-3 play key roles in suppressing T-cell activation. Check for active clinical trials using this agent. (NCI Thesaurus) Link to National Cancer Institute MGD019 bispecific PD-1 x CTLA-4 DART® According to the NCI website, anti-PD-1/anti-CTLA-4 DART protein MGD019 is a hinge stabilized immunoglobulin G4 (IgG4) tetravalent bispecific antibody-like protein directed against the human negative immunoregulatory checkpoint receptors programmed cell death protein 1 (PD-1; PDCD1; CD279) and cytotoxic T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, the anti-PD-1/anti-CTLA4 dual- affinity re-targeting (DART) protein MGD019 specifically binds to both PD-1 and CTLA4 expressed on tumor-infiltrating lymphocytes (TILs) and inhibits the PD-1- and CTLA4-mediated downregulation of T- cell activation and proliferation. Dual blockade of PD1 and CTLA4 pathways provides enhanced activity against PD1+CTLA4+ double positive cells and may increase T-cell activation and proliferation compared to the blockade of either immune checkpoint alone. Check for active clinical trials using this agent. (NCI Thesaurus) More Information in English: Inxight: Drugs (NIH) AdisInsight Link to National Cancer Institute Mechlorethamine According to the NCI the hydrochloride salt of mechlorethamine, is a nitrogen mustard and an analogue of sulfur mustard, with antineoplastic and immunosuppressive activities. Mechlorethamine is metabolized to an unstable, highly reactive ethyleniminium intemediate that alkylates DNA, particularly the 7 nitrogen of guanine residues, resulting in DNA base pair mismatching, DNA interstrand crosslinking, the inhibition of DNA repair and synthesis, cell-cycle arrest, and apoptosis. Indikationen/Anwendungsmöglichkeiten gemäss Chemocare.com: As part of combination regimens in treatment of Hodgkin's disease, non-Hodgkin's lymphoma. As palliative chemotherapy in lung and breast cancers. As a lotion to skin lesions of mycosis fungoides (cutaneous T-cell lymphoma). Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health Link to National Cancer Institute Link zu Wiki Link zu PharmaWiki Link to Physicians Desk Reference (PDR) Info for Patients presented by Scott Hamilton from Chemocare.com Zytostatikum Megestrol According to the NCI website Mimicking the action of progesterone, megestrol binds to and activates nuclear progesterone receptors (PRs) in the reproductive system and pituitary. IIndikationen/Anwendungsmöglichkeiten gemäss folgendem Link (Medien Plus): Megestrol tablets are used to relieve the symptoms and reduce the suffering caused by advanced breast cancer and advanced endometrial cancer (cancer that begins in the lining of the uterus). Megestrol suspension is used to treat loss of appetite, malnutrition, and severe weight loss in patients with acquired immunodeficiency syndrome (AIDS). Megestrol should not be used to prevent loss of appetite and severe weight loss in patients who have not yet developed this condition. Megestrol is a man-made version of the human hormone progesterone. It treats breast cancer and endometrial cancer by affecting female hormones involved in cancer growth. It increases weight gain by increasing appetite. Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health Link to National Cancer Institute Link zu Wiki Link zu PharmaWiki Link to Physicians Desk Reference (PDR) Info for Patients presented by Scott Hamilton from Chemocare.com MEK 162 According to the NCI website the MEK inhibitor MEK162 isan orally available inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/2) with potential antineoplastic activity. MEK inhibitor MEK162, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2. Inhibition of MEK1/2 prevents the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling. This may eventually lead to an inhibition of tumor cell proliferation and an inhibition in production of various inflammatory cytokines including interleukin-1, -6 and tumor necrosis factor. MEK1 and MEK2 are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types. Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health Link to National Cancer Institute Mek inhibitors Melphalan Alkeran® Indikationen/Anwendungsmöglichkeiten gemäss Arzneimittel-Kompendium der Schweiz®: Multiples Myelom. Fortgeschrittenes Ovarialkarzinom. Mammakarzinom. Alkeran kann in Mono- oder Kombinationstherapie beim fortgeschrittenen Mamma-Karzinom eine therapeutische Wirkung haben. Regionale arterielle Perfusion bei lokalisiertem, malignem Melanom oder Weichteilsarkom der Extremitäten. Polycythaemia rubra vera: Alkeran hat sich bei einigen Patienten als wirksam erwiesen.